ANTIFUNGAL & ANTIPARASITIC DRUGS

1. Fungi 2. Protozoa 3. Helminthes (worms) Prevalent in third world countries like the Philippines

FUNGI
Can be found in air, soil, animals, & plants Mycosis (disease caused by fungal infection) Examples: ringworm, athletes foot, candidiasis

ANTIFUNGAL AGENTS
AMPHOTERICIN B
Infections: systemic infections and meningitis caused by candida, cryptococcus and other pathogenic fungi The drug binds with the fungi increasing permeability causing the cell to leak which then leads to loss of cellular components Adverse effects: headache, fever, muscle and joint pain, muscle weakness, GI distress FLUCONAZOLE UTI, pneumonia, mouth and esophagus infections caused by candida Help prevent recurrence of cryptococcal meningitis in AIDS patients Impairs fungal cell membrane by inhibiting enzymes responsible for the synthesis of sterols (steroidlike lipids found in the fungal cell membrane) Adverse effects: headache, GI disturbances Precaution in patients with liver dysfunction as it causes hepatoxicity

FLUCYTOSINE
Endocarditis, UTI, fungemia during candidiasis Meningitis and severe pulmonary infections caused by cryptococcis This drug converts into fluorouracil, an antimetabolite during fungal RNA synthesis. Protein synthesis is impaired which disrupts fungal function Adverse effects: hepatoxicity, bone marrow function impairment (anemia, leukopenia), blood dyscrasias

GRISEOFULVIN
Ringworm, athletes foot This drug inhibits replication because it impairs the mitotic process after binding to the mitotic spindle during cell division Adverse effects: severe headache, GI problems, hypersensitivity, skin photosensitivity

ITRACONAZOLE
Chromomycosis, coccidioidomycosis Works like fluocounazole Adverse effects: headache, GI problems, skin rashes

KETOCONAZOLE
Candidiasis, histoplasmosis, coccidioidomycosis Impairs membrane function by inhibiting sterol synthesis Se: GI disturbances for systemic administration; hepatoxicity, fatal hepatitis on rare occasions Long dosage: gynecomastia (breast tenderness and enlargement due to adrenocorticosteroid synthesis impairment) Thus, replaced by itraconazole

ECHINOCANDINS
Treats esophageal infections caused by candida This drug kills fungus by disrupting cell wall integrity when glucan synthase enzyme (used in biosynthesis of beta-D-glucan) is inhibited SE: headache, GI problems, local irritation at injection site

TERBINAFINE
To treat onychomycosis (toenail and fingernail infections), ringworm Inhibits sterol synthesis SE: hypersensitivity reaction, GI problems, loss of taste (several days after drug is discontinued) If irritation occurs, discontinue drug

VORICONAZOLE
Treats aspergillosis Inhibits sterol synthesis SE: skin rash, blurred vision, seeing bright spots (transient though) Liver toxicity and cardiac arrhythmia if patient is susceptible

PROTOZOA
Single-cell organisms which can cause parasitic infection in humans Common example: MALARIA (caused by parasite known as plasmodia) Another example: dysentery (an intestinal infection)

ANTIMALARIAL AGENTS: CHLOROQUINE

Also treats amoebiasis, RA, SLE This agent impairs metabolic and digestive function of the protozoa SE: retinal toxicity, visual disturbances, GI problems, irritability, confusion depression, nervousness, rashes, itching, discoloration

HYDROXYCHLOROQUINE
Same as CHLOROQUINE

PRIMAQUINE
Treats malarial relapse It impairs DNA function of the parasite SE: GI problems, headache, visual disturbances More serious SE: hemolytic anemia

PYRIMETHAMINE
Treats and prevents malaria It blocks folic acid production (needed in the production of nucleic and amino acids in the these parasites) SE: GI problems, agranulocytosis, leukopenia, thrombocytopenia, tremors, ataxia, seizures, skin rash, anaphylaxis, liver dysfunction

QUININE
One of the oldest forms of antimalarial chemotherapy SE: headache, visual disturbance, ringing in the ears, nausea, vomiting, abdominal pain, cardiac arrhythmias

DRUGS USED TO TREAT PROTOZOAL INFECTIONS IN THE INTESTINES AND OTHER TISSUES
ATOVAQUONE Treats toxoplasmosis, pneumocystis pneumonia SE: fever, skin rash, cough, headache, GI problems

EMETINE AND DEHYDROEMETINE Dysentery treatment SE: arrhythmias, palpitations, GI problems, muscle ache and weakness, localized myositis IODOQUINOL SE: optic and peripheral neuropathies, muscle weakness, ataxia, GI problems, skin reactions METRONIDAZOLE For amoebiasis, trichomoniasis SE: nausea, vomiting, stomach pain, unpleasant taste in the mouth; hypersensitivity reaction, peripheral neuropathy, hematologic abnormalities, genitourinary problems (low incidence though) NITAZOXANIDE For diarrhea SE: GI problems, headache PAROMOMYCIN SE: GI problems PENTAMIDINE Renal toxicity for systemic administration but returns to function once drug is stopped; hypotension, hypoglycemia, GI problems, blood dyscrasias, local pain and tenderness at the injection site

ANTHELMINTICS
ALBENDAZOLE For GI roundworms and hookworms SE: hepatoxicity if long-term use DIETHYLCARBAMAZINE Roundworm infections SE: headache, malaise, appetite loss, weakness IVERMECTIN To treat onchocerciasis SE: fever, swelling and tenderness of lymph glands, skin rash, itching, joint and muscle pain, MEBENDAZOLE Roundworms and tapeworms SE: mild transient GI problems NICLOSAMIDE Tapeworms Remains in the intestinal lumen thus relatively few side effects OXAMNIQUINE For schistosomes SE: headache, dizziness, drowsiness PRAZIQUANTEL Fluke and tapeworm infections headache, dizziness, GI problems PYRANTEL PAMOATE

 roundworms and pinworms SE: mild GI problems THIABENDAZOLE Trichinosis and roundworm infections SE: GI problems, allergic reactions